glyburide; glibenclamide (Micronase, DiaBeta, Glynase)
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Introduction
Tradename: Micronase, DiaBeta. 2nd generation sulfonylurea.
Indications
- treatment of non insulin-dependent diabetes
- may be useful for gestational diabetes[4]
Contraindications
- NOT recommended if creatinine clearance < 50 mL/min[6]
Dosage
start with 2.5-5 mg PO QD, max 20 mg/day, QD or divided BID
Geriatric patients:
- begin 1.25 mg QD, QD dosing
- not recommended, long 1/2life & risk of hypoglycemia
- glipzide is safer
Tabs: 1.25, 2.5, 5 mg.
Micronized glyburide. Tradename: Glynase Press Tab.
Pharmacokinetics
- onset of action 2-4 hours[2], 15-60 min[3]
- duration up to 24 hours
- > 99% plasma protein binding
- metabolism to 2 active & several inactive metabolites [5, 7]
- active metabolites probably excreted via kidneys[7]
- up to 50% eliminated unchanged in the urine[6]
- biphasic elimination: 1/2 life of terminal phase is 10 hours[2], 5-16 hours[3], prolonged with renal insufficiency
- very little crosses placenta[4]
elimination via liver
elimination via kidney
1/2life = 10 hours
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- risk of hypoglycemia seems to be highest among sulfonylureas
- RR=7.5 vs 2.0 for other sulfonylureas relative to metformin[9]
Drug interactions
- alcohol may cause disulfiram reactions
- thiazides & beta adrenergic receptor antagonists decrease effectiveness of glyburide
- non-steroidal anti-inflammatory agents, warfarin, phenytoin & other highly protein-bound agents may displace glyburide from plasma protein binding & increase toxicity
- hypoglycemia may occur in combination with clarithromycin[8]
- drug interaction(s) of sulfonylureas with warfarin
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of fluroquinolones with sulfonylureas
- drug interaction(s) of macrolides with sulfonylureas
- drug interaction(s) of salicylates with sulfonylureas
- drug interaction(s) of gliptins with sulfonylureas
- drug interaction(s) of fluoroquinolones with hypoglycemic agents
Laboratory
Mechanism of action
More general terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 2.0 2.1 2.2 Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 3.0 3.1 3.2 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ 4.0 4.1 4.2 Prescriber's Letter 7(12):71 2000 Journal Watch 20(24):192, 2000 Langer et al, N Engl J Med 343:1134, 2000
- ↑ Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
- ↑ 6.0 6.1 6.2 Drug Evaluation Monograph, Micromedex
- ↑ 7.0 7.1 Ryberg T et al, Diabetes Car 17(9): 1026, 1994 PMID: https://www.ncbi.nlm.nih.gov/pubmed/95079919
- ↑ 8.0 8.1 Paauw DS Dangerous and Deadly Drug Combinations Medscape. June 30, 2016 http://www.medscape.com/features/slideshow/dangerous-drug-combinations
- ↑ 9.0 9.1 van Dalem J et al Risk of hypoglycaemia in users of sulphonylureas compared with metformin in relation to renal function and sulphonylurea metabolite group: population based cohort study. BMJ 2016;354:i3625 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27413017 Free full text <Internet> http://www.bmj.com/content/354/bmj.i3625